This invention relates to the novel use of 5-phenyl-2-furan esters, amides and ketones as neuroprotective agents.
Neuronal death or degeneration occurs continually in mature mammals, including man. It can be accelerated for a variety of reasons including, but not limited to: exposure to neurotoxins, neurodegenerative diseases, trauma, and cerebrovascular accidents such as stroke.
Stroke is the most common life-threatening neurologic disease and is the third leading cause of death in the United States after heart disease and cancer. The American Heart Association estimates that there will be approximately 500,000 new victims of stroke each year.
There currently are no specific therapies to prevent or limit neuronal death or degeneration after ischemia, stroke and in neurodegenerative disorders such as Alzheimer's disease and Huntington's chorea. Accordingly, the method of this invention provides a novel therapeutic approach to prevent or limit neuronal death or degeneration. It has been discovered that 5-phenyl-2-furan esters, amides and ketones possess neuroprotective activity.
A number of phenyl furans are described in the literature. However, these compounds have never been suggested to have neuroprotective activity. For example, U.S. Pat. No. 3,856,825 issued to Wright et al. on Dec. 24, 1974, discloses a series of 3-diethylamino-2,2-dimethylpropyl 5-(substituted phenyl)-2-furoates that possess pharmacological properties, particularly being useful as antispasmodics. U.S. Pat. No. 4,162,257 issued to Pelosi and Yu on Jul. 24, 1979, discloses N,N-dimethyl-5-phenyl-2-furamides said to be useful as anti-inflammatory agents. Oleinik, A. F., "Synthesis and Tuberculostatic Activity of 5-Arylpyromucic Acid Derivatives", Pharmaceutical Chemical Journal. Vol. 10, No. 4 (April 1976), pages 463-465, discloses certain 5-phenyl-2-furans said to have bacteriostatic activity.